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1. 发明申请

WO2013106433A1 CELLULOSE DERIVATIVES FOR INHIBITING CRYSTALLIZATION OF POORLY WATER-SOLUBLE DRUGS 审中-公开
标题翻译：用于抑制不溶性水溶性药物结晶的纤维素衍生物
公开(公告)号：WO2013106433A1
公开(公告)日：2013-07-18
申请号：PCT/US2013/020835
申请日：2013-01-09
申请人： VIRGINIA TECH INTELLECTUAL PROPERTIES, INC. , PERDUE RESEARCH FOUNDATION
发明人： EDGAR, Kevin, J. , LI, Bin , TAYLOR, Lynne , ILEVBARE, Grace , WILLIAMS, Stephanie, M. , LIU, Haoyu
IPC分类号： A61K47/38 , A61K47/30 , A61K9/08 , A61K31/70
CPC分类号： A61K47/38 , A61K9/146 , A61K31/05 , A61K31/352 , A61K31/357 , A61K31/40 , A61K31/427 , A61K31/536 , A61K31/70 , C08B3/00
摘要： The present invention relates to the fields of chemistry and pharmaceuticals. Embodiments of the invention provide cellulose esters useful for inhibiting solution crystallization of drugs. Specific polymers of the invention include cellulose esters of formula (I) : wherein n of the ω-carboxyalkanoyl group, Formula (II), is 3, 4, 6, or 8 to provide a ω-carboxyalkanoyl group chosen from succinoyl, glutaroyl, adipoyl, sebacyl, and suberyl groups; and wherein R is chosen from : a hydrogen atom; and an alkanoyl group chosen from acetyl, propionyl, butyryl, valeroyl, hexanoyl, nonanoyl, decanoyl, lauroyl, palmitoyl, and stearoyl groups; wherein there is a total degree of substitution of the alkanoyl group and the ω-carboxyalkanoyl group of at least 2.0; and wherein the polymer comprises m repeating units where n = 1 to 1,000,000, or 10 to 100,000, or 100 to 1,000, such as 1 to 6,000. Embodiments further include compositions comprising cellulose esters and poorly water-soluble drugs, which compositions exhibit greater solubility and stability in solution as compared to the drugs alone. Drugs that can be used in combination with such polymers include but are not limited to ritonavir, efavirenz, etravirine, celecoxib, clarithromycin, curcumin, ellagic acid, quercetin, naringenin, and resveratrol. Methods for making and using the compounds and compositions are also included within the scope of the invention.
摘要翻译：本发明涉及化学和药物领域。本发明的实施方案提供了可用于抑制药物溶液结晶的纤维素酯。本发明的具体聚合物包括式（I）的纤维素酯：其中式（II）的ω-羧基烷酰基中的n为3,4,6或8，以提供选自琥珀酰基，戊酰基，己二酰基，癸二酰基和辛二酸基; 并且其中R选自：氢原子; 和选自乙酰基，丙酰基，丁酰基，戊酰基，己酰基，壬酰基，癸酰基，月桂酰基，棕榈酰基和硬脂酰基的烷酰基; 其中烷酰基和ω-羧基烷酰基的总取代度为至少2.0; 并且其中所述聚合物包含m个重复单元，其中n = 1至1,000,000，或10至100,000，或100至1,000，如1至6,000。实施方案还包括包含纤维素酯和水溶性差的药物的组合物，与单独的药物相比，该组合物在溶液中表现出更大的溶解度和稳定性。可以与这些聚合物组合使用的药物包括但不限于利托那韦，依法韦仑，依伐维林，塞来昔布，克拉霉素，姜黄素，鞣花酸，槲皮素，柚皮苷和白藜芦醇。制备和使用化合物和组合物的方法也包括在本发明的范围内。

2. 发明申请

WO2018067181A1 BIBENZOATE COPOLYESTERS AND METHODS TO PRODUCE THEM 审中-公开
标题翻译：联苯双酯共聚酯及其制备方法
公开(公告)号：WO2018067181A1
公开(公告)日：2018-04-12
申请号：PCT/US2016/056124
申请日：2016-10-07
申请人： EXXONMOBIL CHEMICAL PATENTS, INC. , VIRGINIA TECH INTELLECTUAL PROPERTIES, INC.
发明人： MONDSCHEIN, Ryan J. , LIU, Haoyu , CHEN, Ting , LONG, Timothy E. , TURNER, Richard S.
IPC分类号： C07C69/78 , C08K5/103 , C08L101/00 , C07C69/76
摘要： Bibenzoate copolyesters are based on (4,4'-biphenyl dicarboxylic acid- co -3,4'-biphenyl dicarboxylic acid) as the diacid component, and on an alicyclic diol compound such as 1,4-cyclohexanedimethanol as a portion of the diol component. Copolyesters are based on 4,4'-biphenyl dicarboxylic acid, and/or 3,4'-biphenyl dicarboxylic acid as the diacid component, and may include a multifunctional acid. Copolymers may optionally have an essentially amorphous morphology, high glass transition temperature, high elongation at break, and/or high melting temperature. A method to make the copolyesters controls the characteristics of the copolyester selected from one or a combination of amorphous morphology or degree of crystallinity, Tg, Tm, tensile modulus, flexural modulus, elongation at break, and so on, by selecting the proportions of the 4,4'-biphenyl dicarboxylic acid or ester producing equivalent thereof, 3,4'-biphenyl dicarboxylic acid or ester producing equivalent thereof, and/or the proportion of the 1,4-cyclohexanedimethanol in the diol component.
摘要翻译：二苯甲酸酯共聚酯基于（4,4'-联苯二甲酸 - 共-3,4'-联苯二甲酸）作为二酸组分，并且在脂环族二醇化合物如1,4-环己烷二甲醇作为二醇组分的一部分。共聚酯基于4,4'-联苯二羧酸和/或3,4'-联苯二羧酸作为二酸组分，并且可以包含多官能酸。共聚物可以任选地具有基本无定形的形态，高玻璃化转变温度，高断裂伸长率和/或高熔融温度。通过选择共聚酯的比例来控制选自无定形形态或结晶度，Tg，Tm，拉伸模量，挠曲模量，断裂伸长率等之一或其组合的共聚酯的特性的方法 4,4'-联苯二甲酸或其酯产生当量，3,4'-联苯二甲酸或其产生酯的当量，和/或1,4-环己烷二甲醇在二醇组分中的比例。

3. 发明申请

WO2017112031A1 TEREPHTHALATE-CO-BIBENZOATE POLYESTERS 审中-公开
标题翻译：对苯二甲酸-CO-苯甲酸酯聚酯
公开(公告)号：WO2017112031A1
公开(公告)日：2017-06-29
申请号：PCT/US2016/056158
申请日：2016-10-07
申请人： EXXONMOBIL CHEMICAL PATENTS INC. , VIRGINIA TECH INTELLECTUAL PROPERTIES, INC.
发明人： LIU, Haoyu , MONDSCHEIN, Ryan J. , CHEN, Ting , LONG, Timothy E. , TURNER, Richard S.
IPC分类号： C08G18/42 , D01F8/14 , C08J5/04
CPC分类号： C08G18/42 , C08J5/04 , D01F6/84
摘要： Copolyesters are based on a diacid component containing terephthalate and4,4'-biphenyl dicarboxylate or 3,4'-biphenyl dicarboxylate, and a diol component containing an alkylene diol, e.g., ethylene glycol or NPG, and an alicyclic polyhydroxyl compound, e.g., CHDM. The copolyesters may have a glass transition temperature more than 100°C and mechanical, thermal and/or barrier characteristics at least comparable to some commercially available copolyesters. A method to control the morphology and properties of a copolyester involves contacting diacid and diol components in the presence of a catalyst, selecting proportions of terephthalic and 4,4'-biphenyl dicarboxylic or 3,4'-biphenyl dicarboxylic acids or ester producing equivalents thereof in the diacid component, and selecting the alkylene diol and proportions of the CHDM (or other alicyclic polyhydroxyl compound) and the alkylene diol in the diol component, to obtain the desired morphology and other properties.
摘要翻译：共聚酯基于含有对苯二甲酸酯和4,4'-联苯二羧酸酯或3,4'-联苯二羧酸酯的二酸组分和含有亚烷基二醇如乙二醇或NPG的二醇组分，以及脂环族多羟基化合物，例如CHDM。共聚酯的玻璃化转变温度可以超过100℃，并且机械，热和/或阻隔特性至少与一些市售的共聚酯相当。控制共聚酯形态和性质的方法包括在催化剂存在下使二酸和二醇组分接触，选择比例的对苯二甲酸和4,4'-联苯二羧酸或3,4'-联苯二羧酸或其酯产生的等价物在二元醇组分中选择亚烷基二醇和CHDM（或其它脂环族多羟基化合物）和亚烷基二醇在二醇组分中的比例，以获得所需的形态和其它性质。

4. 发明申请

WO2018097909A1 BIBENZOATE COPOLYESTERS 审中-公开
公开(公告)号：WO2018097909A1
公开(公告)日：2018-05-31
申请号：PCT/US2017/057259
申请日：2017-10-18
申请人： EXXONMOBIL CHEMICAL PATENTS INC. , VIRGINIA TECH INTELLECTUAL PROPERTIES, INC.
发明人： EDLING, Hans Eliot , LIU, Haoyu , MONDSCHEIN, Ryan J. , LONG, Timothy E. , TURNER, S. Richard , CHEN, Ting
IPC分类号： C08J5/04 , C08G63/185 , D01F6/84
CPC分类号： C08G63/185 , C08J5/04 , D01F6/84
摘要： Copolyesters having improved properties based on a diacid component of 4,4'-biphenyl dicarboxylic acid or 3,4'-biphenyl dicarboxylic acid and a mixed diol component, such as 1,4 cyclohexanedimethanol (CHDM) with ethylene glycol or neopentyl glycol (NPG), e.g., poly(4,4'-biphenyl dicarboxylate-(ethylene glycol-co-CHDM)), poly(4,4'-biphenyl dicarboxylate-(NPG-co-CHDM)), poly(3,4'-biphenyl dicarboxylate-(ethylene glycol-co-CHDM)), poly(3,4'-biphenyl dicarboxylate-(NPG-co-CHDM)); methods of making the copolyesters; and shaped articles made of the copolyesters. Also, polyesters based on biphenyl dicarboxylic acid and NPG; methods of making the polyesters; and shaped articles made of the polyesters.

5. 发明申请

WO2018097908A1 DIACID MODIFIED COPOLYESTERS 审中-公开
公开(公告)号：WO2018097908A1
公开(公告)日：2018-05-31
申请号：PCT/US2017/057255
申请日：2017-10-18
申请人： EXXONMOBIL CHEMICAL PATENTS INC. , VIRGINIA TECH INTELLECTUAL PROPERTIES, INC.
发明人： EDLING, Hans, Eliot , LIU, Haoyu , MONDSCHEIN, Ryan, J. , LONG, Timothy, E. , TURNER, S., Richard , CHEN, Ting
IPC分类号： C08J5/04 , C08G63/185 , D01F6/84
摘要： Copolyesters having improved properties based on 1,4 cyclohexanedimethanol (CHDM) or neopentyl glycol (NPG), and a diacid component containing a combination of two diacids selected from 4,4'-biphenyl dicarboxylic acid, 3,4'-biphenyl dicarboxylic acid, and terephthalic acid; methods of making the copolyesters; and shaped articles made of the copolyesters. Also, polyesters based on biphenyl dicarboxylic acid and NPG; methods of making the polyesters; and shaped articles made of the polyesters

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